摘要
目的:研究扎莱普隆片在20名健康志愿者体内的药代动力学特征及相对生物利用度。方法:20名健康男性志愿者采用随机交叉给药方案,分别单剂量口服的扎莱普隆片10mg和对照胶囊,用液-液相萃取后、HPLC-ESI-MS分析方法对血药浓度进行测定,计算两者的药代动力学参数及相对生物利用度。结果:试验片和对照胶囊的血药浓度水平一致。其主要药代动力学参数t_(1/2)分别为1.17±0.19h和1.14±0.12h;t_(max)分别为0.83±0.12h和0.91±0.12h,C_(max)分别为28.47±2.62μg·l^(-1)和28.12±3.44μg·l^(-1),AUC_(0-8)分别为52.83±4.81μg·h·l^(-1)和54.92±8.83μg·h·l^(-1),两制剂的药代动力学参数相近。用面积估算的扎莱普隆片的相对生物利用度F_(0.8)为(98.3±16.5)％,F_(0-∞)为(98.0±16.4)％。结论:扎莱普隆片和对照胶囊的AUC、C_(max)经方差分析和双单侧t-检验表明:两制剂生物等效;t_(max)经非参数法检验,表明两种制剂无显著性差别(P>0.05)。
OBJECTIVE:To study the pharmacokinetics and relative bioavailability of zaleplon in 20 healthy volunteers. METHODS:A single oral dose 10mg zaleplon of reference or test drugs was given to each volunteer according to an open randomized crossover study. The concentrations in plasma were determined by HPLC-ESI-MS method after liquid-liquid extraction methods. RESULT:The main pharmacokinetics parameters of zaleplon were as follows: rt/2were 1.17±0.19h and 1.14±0.12h, tmax were 0.83 ± 0.12h和0.91± 0.12h, Cmax were 28.47 ± 2.62mg.L-1 and 28.12 ± 3.44mg.L-1, AUC0-8 were 52.83 ± 4.81mg.h-l-1 and 54.92± 8.83mg.h.L-1 for test tablet and reference capsule, respectively. The relative bioavailability of F0-8 and F0-∞ were (98.3 ± 16.5) % and (98.0 ± 16.4) %, respectively . CONCLUSION':The result of statistical analysis showed that two formulations were bioequivalent.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
2003年第1期46-49,共4页
The Chinese Journal of Clinical Pharmacology
